Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
9815409 12243 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1185481 12243 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL416736 12243 17 None 1 2 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 5 0.3 CCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
1979 76958 66 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
CHEMBL20835 76958 66 None -2089 7 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm960467d
2551 780 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
298 780 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
488 780 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
CHEMBL965 780 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
DB00411 780 23 None -7 12 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/S0960-894X(00)80538-7
9838581 11857 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183042 11857 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL277014 11857 2 None 4 2 Mouse 6.0 pEC50 = 6.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 1 1 5 0.1 Cc1noc(C2CN=CNC2)n1 10.1021/jm960467d
3652 4022 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
57 4022 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
60809 4022 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL21536 4022 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
DB15357 4022 72 None -1737 9 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm960467d
10703031 11031 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1178347 11031 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL22089 11031 0 None - 1 Mouse 5.0 pEC50 = 5.0 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 196 3 1 6 -0.1 COCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
44589681 184696 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 184696 0 None -12 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 186470 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 186470 1 None -53 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at muscarinic M3 receptorAgonist activity at muscarinic M3 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
306 3387 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3387 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3387 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3387 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3387 18 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3652 4022 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4022 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4022 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4022 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4022 72 None -275 9 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
2551 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
1726 2451 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2451 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2451 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2451 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2451 12 None 2 6 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
2230 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
296 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
CHEMBL7303 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
DB04365 461 55 None -17 9 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm960467d
10375030 13826 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1196670 13826 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL557795 13826 0 None - 1 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 180 2 1 4 -0.1 C#CCOC(=O)C1CCC(N)=NC1 10.1021/jm960467d
2551 780 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
650899 54114 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54114 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54114 10 None -4 5 Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
42599070 15887 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 15887 0 None -316 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598359 15915 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 15915 0 None -100 5 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
2551 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
9308 17557 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL1255785 17557 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 17557 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL292911 17557 16 None 3 9 Rat 6.9 pEC50 = 6.9 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
2551 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
156015300 177008 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177008 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
10012139 13583 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL1194965 13583 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
CHEMBL553602 13583 10 None 2 2 Mouse 4.9 pEC50 = 4.9 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 1 1 4 -0.1 COC(=O)C1CCC(N)=NC1 10.1021/jm960467d
10240891 204368 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL85678 204368 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 140 1 0 3 0.3 CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 780 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
298 780 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
488 780 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
CHEMBL965 780 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
DB00411 780 23 None -7 12 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
42598360 15913 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 15913 0 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9990434 105845 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 105845 0 None -3 3 Human 4.8 pEC50 = 4.8 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156021744 177530 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4648071 177530 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 374 3 1 3 4.8 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
92209180 13027 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
9793884 13027 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1190710 13027 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL541398 13027 7 None 2 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 156 2 1 4 -0.2 CCOC(=O)C1CN=CNC1 10.1021/jm960467d
124300908 13068 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2606 13068 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1191029 13068 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL542065 13068 5 None 1 2 Mouse 4.8 pEC50 = 4.8 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 166 2 1 4 -0.6 C#CCOC(=O)C1CN=CNC1 10.1021/jm960467d
2551 780 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
298 780 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
488 780 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
CHEMBL965 780 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
DB00411 780 23 None -7 12 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2006.10.040
156015097 176968 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
CHEMBL4640324 176968 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 3 1 3 4.9 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.0c00297
2551 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598829 15889 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223806 15889 0 None -251 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598828 15912 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 15912 0 None -1584 5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
187 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 253 34 None -1 6 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
2551 780 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2529 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2529 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2529 14 None -3 6 Human 5.7 pEC50 = 5.7 Functional
Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 188075 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188075 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
44158142 188075 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188075 40 None -1 4 Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
2551 780 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
298 780 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
488 780 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
CHEMBL965 780 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
DB00411 780 23 None -7 12 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/acs.jmedchem.0c00297
16071018 15863 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 15863 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 15914 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 15914 0 None -794 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 15863 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 15863 15 None -398 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
3652 4022 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4022 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4022 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4022 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4022 72 None -275 9 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
71792 77983 32 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 77983 32 None -6 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
44251554 6968 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 6968 0 None -1 4 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M3. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with human M3 (Class of assay: confirmatory)
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
44422692 11733 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11733 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11733 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
14235519 16364 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
CHEMBL12378 16364 8 None 4 2 Mouse 5.6 pEC50 = 5.6 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 179 1 0 4 1.1 Cc1noc(C2=CCCN(C)C2)n1 10.1021/jm960467d
187 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 253 34 None -1 6 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9815331 201408 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 201408 1 None 3 5 Rat 8.4 pEC50 = 8.4 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
9883040 100058 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100058 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100058 0 None -3 3 Human 8.4 pEC50 = 8.4 Functional
In vitro functional agonism against M3 muscarinic receptor (PI)In vitro functional agonism against M3 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
2551 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
71737672 2529 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2529 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2529 14 None -5 6 Rat 5.5 pEC50 = 5.5 Functional
Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
42599068 15888 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 15888 0 None -100 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 15933 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 15933 0 None -1258 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
319 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1292 39 None -25 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor A91C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
42598586 15932 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 15932 0 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25207745 15935 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 15935 0 None -398 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80032 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80032 2 None -316 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
16123945 80034 8 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 80034 8 None -794 5 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
156011965 176708 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176708 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 780 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
24865895 95546 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL259662 95546 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL390842 95546 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@H]1COC[C@@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
2551 780 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor N95C/T549C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
319 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
321 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
444031 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
784 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
CHEMBL1346 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
DB00496 1292 39 None -25 6 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/acs.jmedchem.0c00297
2551 780 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
298 780 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
488 780 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
CHEMBL965 780 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
DB00411 780 23 None 2 12 Rat 6.3 pEC50 = 6.3 Functional
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9705115
367 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
5487427 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
8592 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL1900528 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL3305968 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
CHEMBL4650755 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
DB01409 3752 8 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1021/acs.jmedchem.0c00297
10197743 12821 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
92209179 12821 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL1189286 12821 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
CHEMBL538467 12821 9 None - 1 Mouse 4.3 pEC50 = 4.3 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 142 1 1 4 -0.6 COC(=O)C1CN=CNC1 10.1021/jm960467d
2551 780 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 780 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 780 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 780 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 780 23 None -7 12 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
44422699 11731 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182272 11731 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL227378 11731 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 C[C@@H]1COC[C@H](C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
44422692 11733 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL1182296 11733 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
CHEMBL228144 11733 0 None -1 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cellsAgonist activity at human muscarinic M3 receptor expressed in CHO cells
ChEMBL 174 2 0 2 0.5 CC1COCC(C[N+](C)(C)C)O1 10.1016/j.bmc.2006.10.040
10727260 11868 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL1183133 11868 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
CHEMBL281411 11868 0 None 2 2 Mouse 5.2 pEC50 = 5.2 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 212 3 1 6 0.6 CSCc1noc(C2CN=CNC2)n1 10.1021/jm960467d
334 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 234 21 None -144 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 receptor by calcium mobilization assayAgonist activity at human muscarinic M3 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
644390 40156 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 40156 6 None -2 4 Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
156014812 177677 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4647437 177677 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650736 177677 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 389 3 1 2 4.9 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1cccc(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156009673 177669 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4633816 177669 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
CHEMBL4650683 177669 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 407 3 1 2 5.1 C[N+]12CCC(CC1)[C@@H](OC(=O)Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)C2 10.1021/acs.jmedchem.0c00297
156015300 177008 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4640703 177008 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assayAgonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
ChEMBL 362 4 2 3 4.7 O=C(Nc1ccc(F)cc1-c1cccc(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
42598591 15886 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 15886 0 None -125 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 15934 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 15934 0 None -251 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
3008304 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
147230103 179563 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 179563 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
3008304 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
3008304 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 3948 48 None -1 4 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
2551 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor K93C/F550C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
2551 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor V94C/K548C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
135409468 1996 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 1996 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 1996 63 None -13 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
647412 27097 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 27097 9 None -5 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M3. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
24967746 15864 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 15864 0 None -199 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598358 15911 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 15911 0 None -794 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10397133 106566 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL315676 106566 1 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 164 2 0 3 0.3 C#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10397356 120191 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120191 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
10130070 119811 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL352908 119811 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 154 2 0 3 0.7 CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
156011965 176708 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
CHEMBL4636528 176708 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assayAntagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
ChEMBL 380 4 2 3 4.8 O=C(Nc1ccc(F)cc1-c1ccc(F)c(Cl)c1)OCC1CCNCC1 10.1021/acs.jmedchem.0c00297
2551 780 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
298 780 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
488 780 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
CHEMBL965 780 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
DB00411 780 23 None 2 12 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysisAgonist activity at rat M3'(3C)-Xa receptor F92C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1074/jbc.m704875200
10375322 58407 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL168545 58407 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptorEffective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor
ChEMBL 192 2 0 3 1.1 CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
2551 780 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
298 780 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
488 780 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
CHEMBL965 780 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
DB00411 780 23 None -93 12 Mouse 5.0 pEC50 = 5 Functional
Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell lineTested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960467d
2551 780 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
298 780 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
488 780 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
CHEMBL965 780 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
DB00411 780 23 None -7 12 Human 7.0 pED50 = 7 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm960683m
5487543 203923 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
CHEMBL81878 203923 4 None -41 6 Human 5.4 pED50 = 5.4 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CCC2C3)c1 10.1021/jm960683m
9795428 96028 4 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
CHEMBL262455 96028 4 None -20 5 Human 6.1 pED50 = 6.1 Functional
Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effectAmplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect
ChEMBL 270 3 0 4 1.8 COc1cccc(C#CCO/N=C2\CN3CC[C@@H]2C3)c1 10.1021/jm960683m
11442478 105983 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085073 105983 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140113 105983 0 None 1 3 Human 9.0 pIC50 = 9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 4 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL5074216 212534 0 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074599 212538 0 None - 1 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5074216 212534 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@@H]3CCN(C)C3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 213243 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44589585 188295 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507375 188295 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555474 188295 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 577 10 4 5 4.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCC[N+](C)(Cc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5074599 212538 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)O[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232700 106016 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3084399 106016 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
CHEMBL3140218 106016 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 364 4 1 1 4.9 Cc1ccccc1C(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)[N+]2(C)C)c1ccccc1C 10.1021/jm900736e
11341753 186710 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492978 186710 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 8 2 4 4.1 CCOc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11341940 186769 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
CHEMBL493328 186769 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 6 2 5 3.8 CC1CN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CCN1 10.1016/j.bmcl.2009.01.098
11364721 192112 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522020 192112 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 7 2 4 3.9 CC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44589495 185388 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL486982 185388 0 None 10 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 5 7 3.8 CCCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590173 188492 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL510029 188492 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL555019 188492 0 None -1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076886 212686 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3C[C@H]4CC[C@H](C3)N4C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
71452454 83490 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206587 83490 0 None 41 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 603 9 3 7 3.9 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CC[N+](C)(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2012.09.085
11552174 103013 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085090 103013 0 None 1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11330061 186719 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492997 186719 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2009.01.098
44589570 172178 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL451040 172178 0 None 15 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 568 10 5 6 3.5 CC(C)NC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589498 172179 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
CHEMBL451043 172179 0 None 3 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 572 11 5 7 3.8 O=C(Nc1ccc(C(=O)OCC2CC2)cc1)N[C@@H](Cc1ccc(O)cc1)C(=O)NC1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.09.020
44573500 187127 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
CHEMBL495361 187127 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 419 6 2 3 4.3 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1ccccc1Cl 10.1016/j.bmcl.2009.01.098
44589575 175060 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL458105 175060 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 596 9 4 7 2.9 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)N4CCOCC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
145955917 161921 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4167221 161921 0 None -29 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 418 6 2 4 4.2 NC[C@H]1CC[C@H](CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44233187 85584 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2306159 85584 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233187 85584 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2306159 85584 0 None -2 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 474 8 1 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNS(=O)(=O)c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324336 103009 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085086 103009 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 370 4 0 4 4.8 Cc1ccsc1CN(C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1016/j.bmcl.2007.09.071
76331543 103015 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085092 103015 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 362 4 0 4 4.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
57758637 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3084466 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
CHEMBL3140183 106004 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysisAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium mobilization by FLIPR analysis
ChEMBL 441 7 0 1 7.2 C[N+]1(CCC2CCCCC2)[C@H]2CC[C@@H]1C[C@H](CC(C#N)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2012.02.015
44232702 106008 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3084401 106008 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
CHEMBL3140203 106008 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 372 4 1 1 4.6 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cccc(F)c1)c1cccc(F)c1)C2 10.1021/jm900736e
11547053 105971 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085074 105971 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140097 105971 0 None -1 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 377 4 0 3 5.0 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(CC1CCCCC1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
145958296 161720 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4164075 161720 0 None -38 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.4 C/C(=C/CN)CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
142416754 161780 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
CHEMBL4164874 161780 0 None -112 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 480 8 2 4 5.2 FC1(F)CCC(NC/C=C\CN(C[C@H]2Cc3ccccc3CN2)[C@H]2CCCc3cccnc32)CC1 10.1021/acsmedchemlett.7b00406
44232708 105991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3084407 105991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
CHEMBL3140145 105991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 408 4 1 1 4.9 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1cc(F)cc(F)c1)c1cc(F)cc(F)c1)C2 10.1021/jm900736e
76320693 103005 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085082 103005 0 None 1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 428 4 0 3 5.2 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccccc1Br)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
76309756 103006 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085083 103006 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 375 4 0 4 4.3 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44590174 169479 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444300 169479 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL466271 169479 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 651 10 3 6 4.6 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(Br)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590177 188325 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507874 188325 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554918 188325 0 None -5 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 677 12 3 7 5.1 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C(=O)c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL5076535 212664 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OCCN(C)C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
11699452 12497 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL1187080 12497 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
CHEMBL489626 12497 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 456 8 1 2 5.8 Cc1ccc(C(O)(c2ccc(C)cc2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)cc1 10.1021/jm801601v
44590179 172138 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL450538 172138 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553446 172138 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 607 10 3 6 4.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccccc2Cl)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44573621 186619 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492391 186619 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 477 8 2 4 5.5 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2009.01.098
44573263 192538 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
CHEMBL522992 192538 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 459 7 2 6 3.4 COc1ccc(CN2CCNCC2)cc1-c1cccc(CNC(=O)c2ccc3c(c2)OCO3)c1 10.1016/j.bmcl.2009.01.098
44590181 172982 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL453248 172982 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL551113 172982 0 None -25 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 633 12 3 8 3.9 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(OC)c(OC)c2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
162646559 179050 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
CHEMBL4742997 179050 0 None -97 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 406 5 0 4 4.1 Cc1cc(F)cnc1N1CCN(C(=O)CCCc2cccc3ncccc23)[C@@H](C)C1 10.1021/acsmedchemlett.0c00626
71459724 83579 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2207177 83579 0 None 63 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 621 10 3 5 5.6 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N2CCC[C@@H]([N+](C)(C)Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2012.09.085
42626092 12511 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL1187132 12511 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
CHEMBL491246 12511 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 8 1 2 5.4 Cc1ccccc1COCC[N+]12CCC(C(O)(c3ccccc3)c3ccccc3)(CC1)CC2 10.1021/jm801601v
145956824 161699 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
CHEMBL4163770 161699 0 None -1412 2 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secsAntagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
ChEMBL 376 6 2 4 3.1 NCC1CC1CN(C[C@H]1Cc2ccccc2CN1)[C@H]1CCCc2cccnc21 10.1021/acsmedchemlett.7b00406
44233417 85605 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL2307674 85605 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233417 85605 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL2307674 85605 0 None -1 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 467 8 2 2 5.7 CN1[C@H]2CC[C@@H]1C[C@H](CC(CNC(=O)NCc1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
76324303 102761 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084394 102761 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 335 5 1 2 4.6 CN1[C@H]2CC[C@@H]1C[C@H](CCC(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
76327870 102764 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
CHEMBL3084397 102764 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 273 4 1 2 3.5 CCC(O)(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)c1ccccc1 10.1021/jm900736e
76327903 103016 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085093 103016 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 381 4 0 5 4.4 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccc(C#N)cc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
76316969 106028 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085075 106028 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140262 106028 0 None -2 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 396 4 0 4 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1cccc(C#N)c1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
71455969 83502 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206603 83502 0 None 3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 581 12 4 5 4.7 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
1765112 102760 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084393 102760 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 307 3 1 2 3.8 CN1[C@H]2CC[C@@H]1C[C@H](C(O)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
25034111 192805 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL526009 192805 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
16040727 168865 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL442672 168865 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL495102 168865 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 649 11 3 6 5.5 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590124 169216 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL443925 169216 0 None 39 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 598 10 4 6 4.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590172 169739 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL444688 169739 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL527216 169739 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 591 10 3 6 4.0 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590171 178161 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL468609 178161 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL554632 178161 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 587 10 3 6 4.2 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
44590125 183269 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480878 183269 0 None 12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 530 10 4 6 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44590170 187777 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL501348 187777 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL553431 187777 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 588 10 4 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N[C@H]2CC[N+](C)(Cc3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2008.09.020
25034111 192805 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL526009 192805 0 None 7 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
76309754 106026 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3085062 106026 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
CHEMBL3140260 106026 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 395 5 0 3 4.6 COc1ccc(CN(C(=O)O[C@@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)cc1 10.1016/j.bmcl.2007.09.071
44589571 172008 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL448904 172008 0 None 10 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 580 11 5 6 3.5 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCC4CC4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
71452456 83508 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206609 83508 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 525 10 4 5 3.8 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC[N+]2(C)CCCCCC2)cc1 10.1016/j.bmcl.2012.09.085
25034180 187818 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL502000 187818 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573744 187056 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
CHEMBL494996 187056 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 457 7 1 5 4.2 CCN1CCN(Cc2cccc(-c3cccc(CNC(=O)c4ccc5c(c4)OCO5)c3)c2)CC1 10.1016/j.bmcl.2009.01.098
44589573 188308 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL507581 188308 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 616 11 5 6 4.3 N#Cc1ccc(CN2CCC(NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)Nc3ccc(C(=O)NCc4ccccc4)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
11510358 105989 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085069 105989 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140143 105989 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 355 4 0 3 4.2 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccoc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44232947 105974 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3084411 105974 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
CHEMBL3140100 105974 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 348 4 1 3 4.5 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccsc1)c1ccsc1)C2 10.1021/jm900736e
11664153 12633 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL1187845 12633 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
CHEMBL523767 12633 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 488 10 1 4 5.2 COc1cccc(C(O)(c2cccc(OC)c2)C23CC[N+](CCOCc4ccccc4)(CC2)CC3)c1 10.1021/jm801601v
76324304 102762 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
CHEMBL3084395 102762 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 322 4 1 3 3.6 CN1[C@H]2CC[C@@H]1C[C@H](CC(O)(c1ccccc1)c1ccccn1)C2 10.1021/jm900736e
15945874 188169 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL505452 188169 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
44573578 186614 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL492374 186614 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 443 7 2 5 3.5 COC(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11455956 187008 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494749 187008 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 463 7 2 5 3.1 CS(=O)(=O)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44590033 183086 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL480299 183086 0 None 12 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 560 11 4 7 3.7 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
15945874 188169 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL505452 188169 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3ccc(O)cc3)C2)cc1 10.1016/j.bmcl.2008.09.020
44589984 189954 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
CHEMBL518001 189954 0 None 7 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(Cc3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2008.09.020
1201549 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
333 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
7601 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL1201203 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL438151 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
DB00245 590 22 None -9 20 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 minsAntagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.0c00626
CHEMBL5076445 212660 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CCN3C)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5078006 212747 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC[C@H]3CN4CCC3CC4)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
CHEMBL5086393 213243 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contractionAntagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
ChEMBL None None None COc1ccc([C@H](Cc2c(Cl)c[n+]([O-])cc2Cl)OC(=O)c2ccc(CNC(C(=O)OC3CCN(C)CC3)c3ccccc3)s2)cc1OC 10.1021/acs.jmedchem.1c00204
44232953 102903 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
CHEMBL3084663 102903 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1021/jm900736e
44232953 102903 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
CHEMBL3084663 102903 0 None -1 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 405 7 2 2 4.6 CCNC(=O)NCC(C[C@@H]1C[C@@H]2CC[C@H](C1)N2C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.07.006
71459689 83488 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
CHEMBL2206585 83488 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 595 13 4 5 5.1 CC(C)OC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCCC[N+](C)(C)Cc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2012.09.085
44573264 186609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
CHEMBL492359 186609 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 447 6 2 5 3.6 O=C(NCc1cccc(-c2ccc(F)c(CN3CCNCC3)c2)c1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2009.01.098
44573619 187009 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494752 187009 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 442 7 3 4 3.6 CC(=O)Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11714747 187040 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494950 187040 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 428 7 2 4 3.8 CN(C)c1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
11578568 187041 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
CHEMBL494951 187041 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 6 3 4 3.3 Nc1cccc(C(=O)NCc2cccc(-c3cccc(CN4CCNCC4)c3)c2)c1 10.1016/j.bmcl.2009.01.098
44573661 187787 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
CHEMBL501486 187787 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 3 4 3.4 O=C(NCc1cccc(-c2cccc(CN3CCNCC3)c2)c1)c1cccc(O)c1 10.1016/j.bmcl.2009.01.098
25034112 187799 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
CHEMBL501727 187799 0 None -1 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assayAntagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 546 10 5 7 3.4 CCOC(=O)c1ccc(NC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H]2CCN(Cc3ccc(O)cc3)C2)cc1 10.1021/jm800634k
11690968 106006 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085072 106006 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140185 106006 0 None 1 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1ccccc1)c1ccsc1)C2 10.1016/j.bmcl.2007.09.071
11518068 106011 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085059 106011 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140213 106011 0 None 1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
11583262 106002 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085060 106002 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3140181 106002 0 None -1 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 371 4 0 3 4.7 C[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)N(Cc1ccsc1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
69444105 102999 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
CHEMBL3085077 102999 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 356 4 0 4 4.5 CN1[C@H]2CC[C@@H]1C[C@@H](OC(=O)N(Cc1cccs1)c1ccccc1)C2 10.1016/j.bmcl.2007.09.071
44233675 102890 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
CHEMBL3084639 102890 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1021/jm900736e
44233675 102890 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
CHEMBL3084639 102890 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPRAntagonist activity against human cloned muscarinic M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL 381 5 0 1 6.3 CN1[C@H]2CC[C@@H]1C[C@H](CC(c1ccccc1)(c1ccccc1)c1ccccc1)C2 10.1016/j.bmcl.2009.07.006
11712408 106027 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3085067 106027 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071
CHEMBL3140261 106027 0 None -1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilizationAntagonist activity at cloned muscarinic M3 receptor expressed in CHO cells by measuring calcium mobilization
ChEMBL 385 4 0 3 5.0 Cc1ccc(CN(C(=O)O[C@H]2C[C@@H]3CC[C@H](C2)[N+]3(C)C)c2ccccc2)s1 10.1016/j.bmcl.2007.09.071